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ID: ALA1133918

Journal: Bioorg Med Chem Lett

Title: Design, synthesis and antiproliferative activity of tripentones: a new series of antitubulin agents.

Authors: Lisowski V, Enguehard C, Lancelot J, Caignard D, Lambel S, Leonce S, Pierre A, Atassi G, Renard P, Rault S.

Abstract: Structure-activity relationship studies of a new series of tripentones (thieno[2,3-b]pyrrolizin-8-ones), led us to prepare several derivatives with antiproliferative activities. The most promising 3-(3-hydroxy-4-methoxyphenyl)thieno[2,3-b]pyrrolizin-8-one 20 (leukemia L1210, IC(50)=15 nM) was shown to be a potent inhibitor of tubulin polymerization.

CiteXplore: 11514171

DOI: 10.1016/s0960-894x(01)00403-6